title: Identification and optimization of tetrahydro-2H-3-benzazepin-2-ones as squalene synthase inhibitors.
abstract: Novel squalene synthase inhibitors are disclosed. SAR and pharmacological profile of selected compounds are discussed.
authors.affiliation: Bayer Pharma AG, Global Drug Discovery, Medicinal Chemistry Wuppertal, Building 460, D-42096 Wuppertal, Germany. nils.griebenow@bayer.com
authors.forename: Nils
authors.initials: N
authors.lastname: Griebenow
authors.forename: Timo
authors.initials: T
authors.lastname: Flessner
authors.forename: Anja
authors.initials: A
authors.lastname: Buchmueller
authors.forename: Martin
authors.initials: M
authors.lastname: Raabe
authors.forename: Hilmar
authors.initials: H
authors.lastname: Bischoff
authors.forename: Peter
authors.initials: P
authors.lastname: Kolkhof
mesh_terms: D000818:Animals; D001552:Benzazepines / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D018360:Crystallography, X-Ray; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000493:pharmacokinetics; D013186:Farnesyl-Diphosphate Farnesyltransferase / Q000037:antagonists & inhibitors* / Q000378:metabolism; D006801:Humans; D051379:Mice; D008862:Microsomes, Liver / Q000378:metabolism; D008968:Molecular Conformation; D013237:Stereoisomerism; D013329:Structure-Activity Relationship
chemical_list: D001552:Benzazepines; D004791:Enzyme Inhibitors; D013186:Farnesyl-Diphosphate Farnesyltransferase